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Zibotentan(ZD4054)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Zibotentan(ZD4054)图片
CAS NO:186497-07-4
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Zibotentan (ZD4054) (ZD4054) 是一种有效的、选择性的、具有口服活性的内皮素 A (ETA) 受体拮抗剂，Ki 为 13 nM。
Cas No.186497-07-4
别名齐泊腾坦,ZD4054
化学名N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
Canonical SMILESCC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4
分子式C19H16N6O4S
分子量424.43
溶解度≥ 7.2mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ZD4054 is a specific antagonist of the endothelin A receptor.

The autocrine endothelin (ET)-1/endothelin A receptor (ETAR) pathway is an important regulator of several processes involved in ovarian cancer progression.

In vitro: In the human ovarian cancer ETAR positive cell lines, ZD4054 effectively inhibited the basal and ET-1-induced cell proliferation, with the inhibition of AKT and p42/44MAPK phosphorylation, and increased apoptosis, through the inhibition of bcl-2 and activation of caspase-3 and poly(ADP-ribose) polymerase proteins. [1].

In vivo: In HEY ovarian cancer xenografts, ZD4054 inhibited tumor growth to the same degree as paclitaxel. Moreover, ZD4054-dependent tumor growth inhibition was associated with a reduction in proliferation index, MMP-2 expression, and microvessel microvessel density [2].

Clinical trial: The PK and safety profiles of ZD4054 determined in this Chinese patient population are similar to those previously reported. Findings suggest no clinically relevant inter-ethnic differences in ZD4054 disposition between the patient populations analyzed [3].

References:
[1] Morris CD, Rose A, Curwen J, Hughes AM, Wilson DJ, Webb DJ.  Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer. 2005 Jun 20;92(12):2148-52.
[2] Rosanò L, Di Castro V, Spinella F, Nicotra MR, Natali PG, Bagnato A.  ZD4054, a specific antagonist of the endothelin A receptor, inhibits tumor growth and enhances paclitaxel activity in human ovarian carcinoma in vitro and in vivo. Mol Cancer Ther. 2007 Jul;6(7):2003-11.
[3] Li J, Liu Y, Qian J, Wu L, Kemp J, Nii M, Tomkinson H, Zuo Y, Ranson M, Usami M.  Single- and multiple-dose pharmacokinetics, safety and tolerability of zibotentan (ZD4054) in Chinese men with advanced solid tumors. Cancer Chemother Pharmacol. 2012 Jul;70(1):57-63.